MX2023004545A - Compounds and methods for the targeted degradation of androgen receptor protein. - Google Patents
Compounds and methods for the targeted degradation of androgen receptor protein.Info
- Publication number
- MX2023004545A MX2023004545A MX2023004545A MX2023004545A MX2023004545A MX 2023004545 A MX2023004545 A MX 2023004545A MX 2023004545 A MX2023004545 A MX 2023004545A MX 2023004545 A MX2023004545 A MX 2023004545A MX 2023004545 A MX2023004545 A MX 2023004545A
- Authority
- MX
- Mexico
- Prior art keywords
- compounds
- target protein
- androgen receptor
- methods
- present disclosure
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 5
- 102000001307 androgen receptors Human genes 0.000 title abstract 4
- 108010080146 androgen receptors Proteins 0.000 title abstract 4
- 230000015556 catabolic process Effects 0.000 title abstract 3
- 238000006731 degradation reaction Methods 0.000 title abstract 3
- 238000000034 method Methods 0.000 title 1
- 102000004169 proteins and genes Human genes 0.000 abstract 4
- 108090000623 proteins and genes Proteins 0.000 abstract 4
- 230000001588 bifunctional effect Effects 0.000 abstract 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 230000005764 inhibitory process Effects 0.000 abstract 2
- 102100032783 Protein cereblon Human genes 0.000 abstract 1
- 102000006275 Ubiquitin-Protein Ligases Human genes 0.000 abstract 1
- 108010083111 Ubiquitin-Protein Ligases Proteins 0.000 abstract 1
- 230000001594 aberrant effect Effects 0.000 abstract 1
- 230000033228 biological regulation Effects 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 230000000144 pharmacologic effect Effects 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
- A61K47/545—Heterocyclic compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
- A61K47/55—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/08—Bridged systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/10—Spiro-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Peptides Or Proteins (AREA)
- Molecular Biology (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
Bifunctional compounds, which find utility as modulators of androgen receptor (AR), are described herein. In particular, the bifunctional compounds of the present disclosure contain on one end a moiety that binds to the cereblon E3 ubiquitin ligase and on the other end a moiety which binds AR, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The bifunctional compounds of the present disclosure exhibit a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aberrant regulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US202063094554P | 2020-10-21 | 2020-10-21 | |
PCT/US2021/055836 WO2022087125A1 (en) | 2020-10-21 | 2021-10-20 | Compounds and methods for the targeted degradation of androgen receptor protein |
Publications (1)
Publication Number | Publication Date |
---|---|
MX2023004545A true MX2023004545A (en) | 2023-07-05 |
Family
ID=78820180
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
MX2023004545A MX2023004545A (en) | 2020-10-21 | 2021-10-20 | Compounds and methods for the targeted degradation of androgen receptor protein. |
Country Status (10)
Country | Link |
---|---|
US (1) | US20230084249A1 (en) |
EP (1) | EP4232445A1 (en) |
JP (1) | JP2023547084A (en) |
KR (1) | KR20230111615A (en) |
CN (1) | CN116783179A (en) |
AU (1) | AU2021365850A1 (en) |
CA (1) | CA3199074A1 (en) |
IL (1) | IL302137A (en) |
MX (1) | MX2023004545A (en) |
WO (1) | WO2022087125A1 (en) |
Families Citing this family (10)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US10584101B2 (en) | 2016-10-11 | 2020-03-10 | Arvinas, Inc. | Compounds and methods for the targeted degradation of androgen receptor |
JP2022532342A (en) | 2019-05-14 | 2022-07-14 | ニューベイション・バイオ・インコーポレイテッド | Anti-cancer nuclear hormone receptor targeting compound |
EP4058464A1 (en) | 2019-11-13 | 2022-09-21 | Nuvation Bio Inc. | Anti-cancer nuclear hormone receptor-targeting compounds |
MX2023011241A (en) | 2021-03-23 | 2023-10-03 | Nuvation Bio Inc | Anti-cancer nuclear hormone receptor-targeting compounds. |
EP4334314A1 (en) | 2021-05-03 | 2024-03-13 | Nuvation Bio Inc. | Anti-cancer nuclear hormone receptor-targeting compounds |
WO2023025268A1 (en) * | 2021-08-27 | 2023-03-02 | 苏州晶云药物科技股份有限公司 | Crystal forms of pyridazine carboxamide compound and preparation method thereof |
AU2022370021A1 (en) * | 2021-10-22 | 2024-05-09 | Gluetacs Therapeutics (Shanghai) Co., Ltd. | Crbn e3 ligase ligand compound, protein degrading agent developed on the basis of ligand compound, and their applications |
US20240018149A1 (en) * | 2022-06-30 | 2024-01-18 | Chu-Chiang Chen | Protein degradation compounds and methods of use |
WO2024012570A1 (en) * | 2022-07-15 | 2024-01-18 | 西藏海思科制药有限公司 | Nitrogen-containing heterocyclic derivative, and composition and pharmaceutical use thereof |
WO2024054952A1 (en) * | 2022-09-08 | 2024-03-14 | Halda Therapeutics Opco, Inc. | Heterobifunctional compounds and methods of treating disease |
Family Cites Families (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4522811A (en) | 1982-07-08 | 1985-06-11 | Syntex (U.S.A.) Inc. | Serial injection of muramyldipeptides and liposomes enhances the anti-infective activity of muramyldipeptides |
EP2802608A4 (en) | 2012-01-12 | 2015-08-05 | Univ Yale | Compounds&methods for the enhanced degradation of targeted proteins&other polypeptides by an e3 ubiquitin ligase |
US20160058872A1 (en) | 2014-04-14 | 2016-03-03 | Arvinas, Inc. | Imide-based modulators of proteolysis and associated methods of use |
KR20210132233A (en) | 2014-04-14 | 2021-11-03 | 아비나스 오퍼레이션스, 인코포레이티드 | Imide-based modulators of proteolysis and associated methods of use |
US20180228907A1 (en) | 2014-04-14 | 2018-08-16 | Arvinas, Inc. | Cereblon ligands and bifunctional compounds comprising the same |
US10584101B2 (en) * | 2016-10-11 | 2020-03-10 | Arvinas, Inc. | Compounds and methods for the targeted degradation of androgen receptor |
-
2021
- 2021-10-20 US US17/506,324 patent/US20230084249A1/en active Pending
- 2021-10-20 KR KR1020237016862A patent/KR20230111615A/en unknown
- 2021-10-20 AU AU2021365850A patent/AU2021365850A1/en active Pending
- 2021-10-20 CA CA3199074A patent/CA3199074A1/en active Pending
- 2021-10-20 MX MX2023004545A patent/MX2023004545A/en unknown
- 2021-10-20 WO PCT/US2021/055836 patent/WO2022087125A1/en active Application Filing
- 2021-10-20 CN CN202180078059.0A patent/CN116783179A/en active Pending
- 2021-10-20 IL IL302137A patent/IL302137A/en unknown
- 2021-10-20 JP JP2023524281A patent/JP2023547084A/en active Pending
- 2021-10-20 EP EP21816573.6A patent/EP4232445A1/en active Pending
Also Published As
Publication number | Publication date |
---|---|
KR20230111615A (en) | 2023-07-25 |
CA3199074A1 (en) | 2022-04-28 |
JP2023547084A (en) | 2023-11-09 |
CN116783179A (en) | 2023-09-19 |
EP4232445A1 (en) | 2023-08-30 |
IL302137A (en) | 2023-06-01 |
US20230084249A1 (en) | 2023-03-16 |
WO2022087125A1 (en) | 2022-04-28 |
AU2021365850A1 (en) | 2023-06-08 |
Similar Documents
Publication | Publication Date | Title |
---|---|---|
MX2023004545A (en) | Compounds and methods for the targeted degradation of androgen receptor protein. | |
PH12020500663A1 (en) | Brm targeting compounds and associated methods of use | |
MX2022010583A (en) | Tetrahydronaphthalene and tetrahydroisoquinoline derivatives as estrogen receptor degraders. | |
MX2022011674A (en) | Indazole based compounds and associated methods of use. | |
MX2022004526A (en) | Bifunctional molecules containing an e3 ubiquitine ligase binding moiety linked to a bcl6 targeting moiety. | |
EP4234551A3 (en) | Pyridazinones as parp7 inhibitors | |
MX2019005007A (en) | Tau-protein targeting protacs and associated methods of use. | |
CR20230516A (en) | Modulators of bcl6 proteolysis and associated methods of use | |
EP4026835A3 (en) | Pd-1/pd-l1 inhibitors | |
MX2021009563A (en) | Pharmaceutical combination comprising tno155 and ribociclib. | |
MX2021009562A (en) | Pharmaceutical combination comprising tno155 and a pd-1 inhibitor. | |
MX2023008031A (en) | Gcn2 inhibitors and uses thereof. | |
PH12020550881A1 (en) | Substituted bicyclic heterocyclic compounds as prmt5 inhibitors | |
MX2023000025A (en) | Hpk1 inhibitors and uses thereof. | |
MY158106A (en) | Inhibitors of e1 activating enzymes | |
WO2022031847A3 (en) | Compositions and methods for inhibiting plp1 expression | |
PH12020551390A1 (en) | AMINOPYRAZINE DIOL COMPOUNDS AS PI3K-y INHIBITORS | |
PH12021500008A1 (en) | Transglutaminase 2 (tg2) inhibitors | |
PH12018500423A1 (en) | Inhibitors of ezh2 | |
WO2023141570A3 (en) | Compounds and methods for the targeted degradation of kras | |
MX2022004759A (en) | Methods and compositions for treating liver diseases and disorders. | |
WO2022218941A3 (en) | Compositions and methods for inhibiting ketohexokinase (khk) | |
MX2022016357A (en) | Tetrazole derivatives as trpa1 inhibitors. | |
MX2022008627A (en) | Substituted pyrazolo-pyrimidines and uses thereof. | |
AU2020378127A8 (en) | Compounds as CD73 inhibitors |